Piperidyl amides, sulfonamides and sulfoxamides as inhibitors of cholesterol biosynthesis

Abstract

The present invention relates to piperidyl amides which are useful as inhibitors of cholesterol biosynthesis and as agents which lower total serum cholesterol in patients in need thereof.

What is claimed is: 
     
       1. A method of inhibiting the biosynthesis of cholesterol in a patient in need thereof comprising administering to said patient an effective cholesterol biosynthesis inhibiting amount of a compound of the formula ##STR16## wherein A is a C 2  -C 14  alkylene; Y is a methylene, oxygen, sulfur, sulfinyl or sulfonyl; B is a C 2  -C 14  alkyl, ##STR17## m is an integer 0 or 1; v is an integer 0, 1 or 2; and   R is --(CH 2 ) m  OH, with the proviso that when m is 0, R cannot be in the 2-position of the piperidine ring or R is a radical of the formula ##STR18## wherein n is an integer 0, 1, 2 or 3; and R 1  is hydrogen, phenyl, vinyl or a C 1  -C 4  alkyl; provided that when R is a radical of the formula ##STR19## or when B is a C 2  -C 14  alkyl and v is 0, Y is not methylene.     
     
     
       2. A method of lowering plasma cholesterol in a patient in need thereof comprising administering to said patient an effective hypocholesterolemic amount of a compound of the formula ##STR20## wherein A is a C 2  -C 14  alkylene; Y is a methylene, oxygen, sulfur, sulfinyl or sulfonyl; B is a C 2  -C 14  alkyl, ##STR21## m is an integer 0 or 1; v is an integer 0, 1 or 2; and   R is --(CH 2 ) m  OH, with the proviso that when m is 0, R cannot be in the 2-position of the piperidine ring or R is a radical of the formula ##STR22## wherein n is an integer 0, 1, 2 or 3; and R 1  is hydrogen, phenyl, vinyl or a C 1  -C 4  alkyl; provided that when R is a radical of the formula ##STR23## or when B is a C 2  -C 14  alkyl and v is 0, Y is not methylene.     
     
     
       3. A method of treating a patient afflicted with hypercholesterolemia comprising administering to said patient an effective hypocholesterolemic amount of a compound of the formula ##STR24## wherein A is a C 2  -C 14  alkylene; Y is a methylene, oxygen, sulfur, sulfinyl or sulfonyl; B is a C 2  -C 14  alkyl, ##STR25## m is an integer 0 or 1; v is an integer 0, 1 or 2; and   R is --(CH 2 ) m  OH, with the proviso that when m is 0, R cannot be in the 2-position of the piperidine ring or R is a radical of the formula ##STR26## wherein n is an integer 0, 1, 2 or 3; and R 1  is hydrogen, phenyl, vinyl or a C 1  -C 4  alkyl; provided that when R is a radical of the formula ##STR27## or when B is a C 2  -C 14  alkyl and v is 0, Y is not methylene.